RG 13022

Catalog No.S2115 Synonyms: Tyrphostin RG13022

For research use only.

RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.

RG 13022 Chemical Structure

CAS No. 136831-48-6

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Biological Activity

Description RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.
Targets
EGFR [1]
(Cell-free assay)
4 μM
In vitro

RG-13022 inhibits autophosphorylation of the EGF-receptor in HER 14 cells after an overnight incubation.The IC50 of RG-13022 is 5 μM. RG-13022 inhibits colony formation and DNA synthesis by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50 for RG-13022 is 1 μM for HER 14 colony formation and 3 μM for HER 14 DNA synthesis. RG-13022 also suppresses colony formation and DNA synthesis by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50 for RG-13022 on MH-85 cells is 7 μM for colony formation and 1.5 μM for DNA synthesis.[1].

In vivo

RG-13022 (400 μg/mouse/day) significantly inhibits MH-85 tumor growth. Because of slower tumor growth, MH-85 tumor-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals. As a result of suppression of tumor growth, RG-13022 prolongs the life span of MH-85 tumor-bearing animals. Administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 μg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice.[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HER14 Cells, MH-85 Cells
  • Concentrations: 0-60 μM
  • Incubation Time: 10 days
  • Method:

    MH-85 cells (100/well; 24-well plate) and HER 14 cells (200/dish; 10-cm dish) are plated in complete medium, either alpha MEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to alpha MEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this medium in the presence or absence of increasing concentrations of RG-13022 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope.

Animal Research:

[1]

  • Animal Models: 4- to 6-week-old male BALB/c nu/nu mice
  • Dosages: 400 μg/mouse/day
  • Administration: IV

Solubility (25°C)

In vitro

DMSO 53 mg/mL
(199.03 mM)
Water Insoluble
Ethanol '5 mg/mL

Chemical Information

Molecular Weight 266.29
Formula

C16H14N2O2

 

CAS No. 136831-48-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C(C=C1)C=C(C#N)C2=CN=CC=C2)OC

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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